Multi-core adhesive microspheres for loading water soluble low molecular medicament and preparation method thereof

A water-soluble small molecule, drug-loading technology, which is applied in the directions of non-active components of polymer compounds, pharmaceutical formulations, and medical preparations with non-active components, etc., to achieve the effect of increasing the drug-loading capacity and reducing leakage

Active Publication Date: 2012-06-20
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Water-insoluble and enteric-soluble acrylic resins can be used as sustained-release materials to control the release of water-soluble small molecule drugs in an acidic environment, but due to their lack of adhesive properties, these two materials are only commonly used as sustained-release materials. Matrix tablet materials and enteric coating materials, but there is no report of using them for gastric retention sustained-release microspheres

Method used

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  • Multi-core adhesive microspheres for loading water soluble low molecular medicament and preparation method thereof
  • Multi-core adhesive microspheres for loading water soluble low molecular medicament and preparation method thereof
  • Multi-core adhesive microspheres for loading water soluble low molecular medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The influence of embodiment 1 prescription on release rate

[0060] Prescription 1

[0061] Evenly disperse 200mg of berberine hydrochloride and 200mg of aluminum stearate in 10ml of 1% acrylic resin No. II containing 5% water in acetone solution, add this mixture to 80ml of acetone saturated liquid paraffin and stir at a speed of 900rpm Form an oil-in-oil emulsion, stir at room temperature for 5 hours to completely evaporate the internal solvent, centrifuge to obtain acrylic resin core microspheres, wash with n-hexane three times to remove residual liquid paraffin, and dry.

[0062] Add 200mg of the acrylic resin microspheres prepared above to 2% acetic acid solution containing 3% (w / v) chitosan and 3% (w / v) gelatin at 40°C, stir to make it evenly dispersed and let stand Degassing, as the water phase; mix 80ml of liquid paraffin and 0.16g of Span80 as the oil phase; keep both the water phase and the oil phase at 40°C, add the water phase to the oil phase, and stir at ...

Embodiment 2

[0071] Example 2 In Vivo Adhesion Research of Multi-core Adhesive Microspheres

[0072] The experimental conditions are: 200g-250g Wistar rats are fasted for 12 hours, and after anesthesia, a small opening is made in the distal esophagus and proximal duodenum and connected with polyethylene tubes respectively. After flushing away the residual contents in the stomach with normal saline, 100 microspheres and 0.2ml of water were infused. Ten minutes later, the stomach was flushed with artificial gastric juice at a flow rate of 1.5ml / min for 1.5h. Record the number of microspheres cleared from the stomach after washing, and calculate the retention percentage.

[0073] Prescription 2, Comparative Example 1 and Comparative Example 2 in Example 1 were selected, and the retention rate in the gastric mucosa was investigated in vivo. The higher the retention rate of the microparticles in the gastric mucosa, the better the adhesion performance of the microspheres, and the higher the dru...

Embodiment 3

[0077] Evenly disperse 100mg of amoxicillin and 200mg of magnesium stearate in 10ml of 1% acrylic resin No. III in acetone solution containing 5% of water, add this mixture to 80ml of acetone-saturated liquid paraffin and stir at a speed of 900rpm to form an oil Oil-in-emulsion, stirred at room temperature for 5 hours to completely evaporate the internal solvent, centrifuged to obtain acrylic resin core microspheres, washed three times with petroleum ether to remove residual liquid paraffin, and dried.

[0078] Add 75 mg of the above-mentioned prepared internal acrylate resin microspheres into 2% acetic acid solution containing 3% (w / v) chitosan and 1.5% (w / v) gelatin at 40°C, stir to make it uniformly dispersed and Stand still for defoaming, as the water phase; mix 80ml of liquid paraffin and 0.16g of Span85 as the oil phase; both the water phase and the oil phase are kept at 40°C, add the water phase to the oil phase, and stir at 600 rpm for 20 minutes to obtain an emulsion ...

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Abstract

The invention discloses multi-core adhesive microspheres capable of loading a water soluble low molecular medicament. The microspheres are ionic cross-linked chitosan / gelatin microspheres, wherein acrylic resin microspheres for wrapping and controlling the releasing of the water soluble low molecular medicament are dispersed in the microspheres. A preparation method comprises the following steps of: dispersing or dissolving the medicament into solution of acrylic resin-containing organic solvent; preparing medicament-loading microsphere cores by an emulsification solvent volatilization method; dispersing the cores in the solution of chitosan and gelatin; preparing W / O type mixture from the mixture and oily ingredients; solidifying the gelatin at a low temperature and separating the microspheres from the oil phase; and finally performing cross linking with ionic cross-linking aqueous solution. The chitosan medicament-loading microspheres have the advantages of controllable particle size distribution, good release control effect of water soluble medicament, adjustable releasing rate, high biological adhesion, simple preparation method, and mild condition.

Description

technical field [0001] The invention relates to a multi-core adhesion microsphere which can be used to load water-soluble small molecule drugs and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background of the invention [0002] Gastric retention preparations are a class of preparations that can prolong the residence time of drugs in the stomach and increase the local concentration of drugs in the gastric mucosa. Gastric retention preparations are a good means of administration for drugs that are absorbed in the stomach or act locally in the stomach, such as antibacterial drugs used to fight ulcers caused by Helicobacter pylori. Gastric-adhesive preparations, which have been considered as a better gastric-retentive drug delivery system in recent years, have been extensively studied. [0003] Chitosan is a copolymer obtained by deacetylation of chitin, which has good biocompatibility. Due to the large number of amino groups in the mol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/42A61K47/32A61K47/36
Inventor 黄园朱晰张志荣
Owner SICHUAN UNIV
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